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Selectivity data for probe BI-9627 and control BI-0054


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BI-9627


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A -5.21
5-HT1B HTR1B 14.55
5-HT1D HTR1D 33.98
5-HT1E HTR1E -9.59
5-HT2A HTR2A -22.65 > 10000.00 < 5.00
5-HT2B HTR2B -8.79
5-HT2C HTR2C 2.59
5-HT3 HTR3A -6.68
5-HT5A HTR5A -4.89
5-HT6 HTR6 1.25
5-HT7A HTR7 16.30
D1 DRD1 -10.25
D2 DRD2 -19.53
D3 DRD3 -13.42
D4 DRD4 -5.70
D5 DRD5 -8.21
SERT SLC6A4 21.39
NET SLC6A2 28.57
DAT SLC6A3 77.86 1523.00 5.80
MOR OPRM1 8.98
DOR OPRD1 -5.35
KOR OPRK1 9.26
GABAA 14.56
H1 HRH1 7.60
H2 HRH2 -11.18
H3 HRH3 -6.54
H4 HRH4 7.11
Alpha1A ADRA1A 6.05
Alpha1B ADRA1B -15.57
Alpha2A ADRA2A -0.34
Alpha2B ADRA2B 6.29
Alpha2C ADRA2C 9.12
Beta1 ADRB1 -9.29
Beta2 ADRB2 -9.75
M1 CHRM1 12.36
M2 CHRM2 23.49
M3 CHRM3 12.09
M4 CHRM4 22.31
M5 CHRM5 -8.36
Beta3 ADRB3 5.47
GABAA/BZP 13.92
GABA/PBR 6.39
Alpha1D ADRA1D 50.00 > 10000.00 < 5.00
Sigma 2 TMEM97 -6.34
Sigma 1 SIGMAR1 -27.86

BI-0054


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A -15.67
5-HT1B HTR1B 37.78
5-HT1D HTR1D 9.64
5-HT1E HTR1E -19.01
5-HT2A HTR2A -11.00
5-HT2B HTR2B -2.75
5-HT2C HTR2C -2.86
5-HT3 HTR3A -4.49
5-HT5A HTR5A -11.51
5-HT6 HTR6 0.27
5-HT7A HTR7 3.32
D1 DRD1 4.80
D2 DRD2 -4.57
D3 DRD3 -7.75
D4 DRD4 -5.64
D5 DRD5 -9.82
SERT SLC6A4 11.78
NET SLC6A2 21.48
DAT SLC6A3 87.29 825.00 6.10
MOR OPRM1 -2.53
DOR OPRD1 -0.82
KOR OPRK1 -13.88
GABAA 16.99
H1 HRH1 -0.16
H2 HRH2 -9.37
H3 HRH3 -17.99
H4 HRH4 9.81
Alpha1A ADRA1A -5.10
Alpha1B ADRA1B -0.60
Alpha2A ADRA2A 4.92
Alpha2B ADRA2B 1.01
Alpha2C ADRA2C 16.27
Beta1 ADRB1 -17.98
Beta2 ADRB2 -14.24
M1 CHRM1 -7.86
M2 CHRM2 -0.80
M3 CHRM3 -10.86
M4 CHRM4 19.88
M5 CHRM5 14.94
Beta3 ADRB3 8.52
GABAA/BZP 25.27
GABA/PBR -2.17
Alpha1D ADRA1D 50.00 > 10000.00 < 5.00
Sigma 2 TMEM97 -0.12
Sigma 1 SIGMAR1 -8.45

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Primary results are shown as '% Ctrl', i.e. the negative control (DMSO) is equal 100% control and the positive control (control compound) is equal 0% control. For compounds showing less than 50% of control in the primary screening assay, a Kd will be determined. Note: It cannot be excluded that 0 % control values are due to assay artefacts.
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BI-9627


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 89.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 93.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 96.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 99.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 96.0 1000
PRKAA1 AMPK-alpha1 97.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 86.0 1000
AURKA AURKA 87.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 96.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 100.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 87.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 85.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 95.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 93.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 92.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 87.0 1000
CDK7 CDK7 86.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 82.0 1000
CHEK1 CHEK1 95.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 98.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 85.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 92.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 95.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 100.0 1000
DCLK2 DCAMKL2 93.0 1000
DCLK3 DCAMKL3 98.0 1000
DDR1 DDR1 83.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 92.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 74.0 1000
DYRK1B DYRK1B 45.0 1000
DYRK2 DYRK2 89.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 99.0 1000
EPHA6 EPHA6 96.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 97.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 92.0 1000
ERBB3 ERBB3 98.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 96.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 100.0 1000
FER FER 96.0 1000
FES FES 96.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 98.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 91.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 89.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 73.0 1000
GRK1 GRK1 98.0 1000
GRK2 GRK2 96.0 1000
GRK3 GRK3 92.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 97.0 1000
GSK3A GSK3A 97.0 1000
GSK3B GSK3B 85.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 81.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 82.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 94.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 70.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 99.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 73.0 1000
MAPK9 JNK2 95.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 95.0 1000
LATS1 LATS1 72.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 91.0 1000
STK11 LKB1 73.0 1000
STK10 LOK 94.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 100.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 79.0 1000
MAP3K1 MAP3K1 96.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 90.0 1000
MAP3K4 MAP3K4 98.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 88.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 49.0 1000
MAP2K1 MEK1 97.0 1000
MAP2K2 MEK2 96.0 1000
MAP2K3 MEK3 100.0 1000
MAP2K4 MEK4 95.0 1000
MAP2K5 MEK5 86.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 81.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 95.0 1000
MAP2K7 MKK7 86.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 95.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 98.0 1000
MST1R MST1R 97.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 97.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 90.0 1000
MYLK2 MYLK2 85.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 96.0 1000
STK38L NDR2 99.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 92.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 79.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 88.0 1000
MAPK13 p38-delta 83.0 1000
MAPK12 p38-gamma 77.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 84.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 91.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 94.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 87.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 95.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 100.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 34.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 84.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 94.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 77.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 87.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 100.0 1000
PLK1 PLK1 90.0 1000
PLK2 PLK2 93.0 1000
PLK3 PLK3 82.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 91.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 80.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 78.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 76.0 1000
DSTYK RIPK5 94.0 1000
ROCK1 ROCK1 87.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 97.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 97.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 100.0 1000
SRMS SRMS 80.0 1000
SRPK1 SRPK1 86.0 1000
SRPK2 SRPK2 0.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 90.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 94.0 1000
TAOK3 TAOK3 86.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 95.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 96.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 89.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 98.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 80.0 1000
KDR VEGFR2 93.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 98.0 1000
WNK3 WNK3 84.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 89.0 1000
STK32C YANK3 100.0 1000
YES1 YES 98.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 100.0 1000

BI-0054


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 83.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 95.0 1000
COQ8B ADCK4 97.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 91.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 70.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 98.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 93.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 94.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 89.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 100.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 88.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 97.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 88.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 94.0 1000
CAMK2B CAMK2B 88.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 92.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 85.0 1000
CDK11B CDC2L1 92.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 89.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 84.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 79.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 91.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 94.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 76.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 95.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 86.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 84.0 1000
DCLK1 DCAMKL1 89.0 1000
DCLK2 DCAMKL2 88.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 96.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 93.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 74.0 1000
DYRK1B DYRK1B 37.0 1000
DYRK2 DYRK2 93.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 83.0 1000
EPHA1 EPHA1 88.0 1000
EPHA2 EPHA2 94.0 1000
EPHA3 EPHA3 95.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 98.0 1000
EPHA7 EPHA7 99.0 1000
EPHA8 EPHA8 93.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 82.0 1000
EPHB3 EPHB3 93.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 94.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 87.0 1000
MAPK7 ERK5 89.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 60.0 1000
PTK2 FAK 17.0 1000
FER FER 93.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 86.0 1000
FGFR3 FGFR3(G697C) 87.0 1000
FGFR4 FGFR4 88.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 98.0 1000
FRK FRK 97.0 1000
FYN FYN 76.0 1000
GAK GAK 97.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 52.0 1000
GRK1 GRK1 95.0 1000
GRK2 GRK2 77.0 1000
GRK3 GRK3 76.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 87.0 1000
GSK3A GSK3A 78.0 1000
GSK3B GSK3B 88.0 1000
HASPIN HASPIN 78.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 91.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 72.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 88.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 90.0 1000
IKBKB IKK-beta 85.0 1000
IKBKE IKK-epsilon 71.0 1000
INSR INSR 100.0 1000
INSRR INSRR 81.0 1000
IRAK1 IRAK1 78.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 89.0 1000
ITK ITK 91.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 84.0 1000
MAPK9 JNK2 92.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 91.0 1000
LATS1 LATS1 93.0 1000
LATS2 LATS2 91.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 98.0 1000
STK11 LKB1 71.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 100.0 1000
LYN LYN 94.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 61.0 1000
MAP3K1 MAP3K1 86.0 1000
MAP3K15 MAP3K15 93.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 81.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 95.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 88.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 87.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 87.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 92.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 80.0 1000
STK3 MST2 100.0 1000
STK24 MST3 97.0 1000
STK26 MST4 89.0 1000
MTOR MTOR 67.0 1000
MUSK MUSK 90.0 1000
MYLK MYLK 90.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 85.0 1000
STK38L NDR2 90.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 93.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 63.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 95.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 98.0 1000
MAPK13 p38-delta 75.0 1000
MAPK12 p38-gamma 55.0 1000
PAK1 PAK1 98.0 1000
PAK2 PAK2 95.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 87.0 1000
CDK16 PCTK1 84.0 1000
CDK17 PCTK2 89.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 92.0 1000
PDGFRB PDGFRB 95.0 1000
PDPK1 PDPK1 94.0 1000
CDPK1 PFCDPK1(P.falciparum) 90.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 50.0 1000
PIK3C2G PIK3C2G 85.0 1000
PIK3CA PIK3CA(Q546K) 100.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 91.0 1000
PIKFYVE PIKFYVE 88.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 99.0 1000
PIP4K2B PIP5K2B 75.0 1000
PIP4K2C PIP5K2C 94.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 100.0 1000
PLK1 PLK1 88.0 1000
PLK2 PLK2 80.0 1000
PLK3 PLK3 78.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 84.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 83.0 1000
PRKCQ PRKCQ 93.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 93.0 1000
RIOK3 RIOK3 98.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 64.0 1000
DSTYK RIPK5 74.0 1000
ROCK1 ROCK1 0.5 1000
ROCK2 ROCK2 73.0 1000
ROS1 ROS1 99.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 81.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 70.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 99.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 83.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 98.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 97.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 82.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 94.0 1000
NUAK2 SNARK 90.0 1000
SNRK SNRK 98.0 1000
SRC SRC 99.0 1000
SRMS SRMS 89.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 83.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 87.0 1000
TBK1 TBK1 98.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 72.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 82.0 1000
TEK TIE2 100.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 68.0 1000
TNK1 TNK1 84.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 98.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 90.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 82.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 89.0 1000
ULK1 ULK1 85.0 1000
ULK2 ULK2 82.0 1000
ULK3 ULK3 89.0 1000
KDR VEGFR2 80.0 1000
PIK3C3 VPS34 88.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 99.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 86.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 100.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 88.0 1000
ZAP70 ZAP70 97.0 1000

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BI-9627

Conclusion: Closest hit is M2 with 67 % inhibition at 10 µM.

Target protein HGNC name Species % control at 10 µM % control at 30 µM % control at 3 µM % control at 1 µM % control at 0.3 µM % control at 0.1 µM Mode of action Assay
5HT1A/HU HTR1A Homo sapiens 82.0 Radioactive Assay
5HT3/HU HTR3A Homo sapiens 98.0 Others
5HTTRANS/HU SLC6A4 Homo sapiens 89.0 Radioactive Assay
A1/HU ADORA1 Homo sapiens 58.0 Radioactive Assay
A2A/HU ADORA2A Homo sapiens 86.0
A3/H ADORA3 Homo sapiens 105.0
ALPHA1A/R ADRA1A Rattus norvegicus 86.0 Others
ALPHA1B/R ADRA1B Rattus norvegicus 95.0 Radioactive Assay
ALPHA1D/H ADRA1D Homo sapiens 98.0 Others
ALPHA2A/H ADRA2A Homo sapiens 93.0 Radioactive Assay
B1/H BDKRB1 Homo sapiens 97.0 Radioactive Assay
B2/HU BDKRB2 Homo sapiens 105.0 Radioactive Assay
BETA1/HU ADRB1 Homo sapiens 102.0 Radioactive Assay
BETA2/HU ADRB2 Homo sapiens 102.0 Radioactive Assay
CA+/DHPSI/RA CACNA1C Rattus norvegicus 77.0 Radioactive Assay
CA+/DILSI/RA CACNA1C Rattus norvegicus 68.0 Radioactive Assay
CA+/N/RA CACNA1B Rattus norvegicus 98.0 Radioactive Assay
CYSLT1_HS CYSLTR1 Homo sapiens 95.0 Radioactive Assay
D1/HU DRD1 Homo sapiens 94.0 Radioactive Assay
D2S/HU DRD2 Homo sapiens 110.0 Radioligand Binding
D3/HU DRD3 Homo sapiens 117.0 Radioactive Assay
D4.2/H DRD4 Homo sapiens 105.0 Radioactive Assay
DATRANS/H SLC6A3 Homo sapiens 101.0 inhibitor Radioactive Assay
DELTA/HU OPRD1 Homo sapiens 113.0 Radioactive Assay
EGF/HU EGFR Homo sapiens 88.0 Radioactive Assay
EP4/H PTGER4 Homo sapiens 99.0 Radioactive Assay
ERALPHA/H ESR1 Homo sapiens 106.0 Radioactive Assay
ETA/HU EDNRA Homo sapiens 103.0 Radioactive Assay
ETB/HUM EDNRB Homo sapiens 114.0 Radioactive Assay
GABAA MUSCIMOL CENT GABRA1 Rattus norvegicus 89.0 Scintillation counting
GABAACENTR GABRA1 Rattus norvegicus 92.0 Radioactive Assay
GABATRANS/RA SLC6A1 Rattus norvegicus 101.0 Radioactive Assay
GABA_B1A GABBR1 Homo sapiens 103.0 Radioactive Assay
GLUCOCORTICO NR3C1 Homo sapiens 98.0 Radioactive Assay
GPR103 QRFPR Homo sapiens 92.0 Radioactive Assay
H1/H HRH1 Homo sapiens 98.0 Radioactive Assay
H2/H HRH2 Homo sapiens 103.0 Radioactive Assay
H3/H HRH3 Homo sapiens 109.0 Radioactive Assay
I2/CENTR/R GNAI2 Rattus norvegicus 88.0 Radioactive Assay
K+/HERG KCNH2 Homo sapiens 105.0 Radioactive Assay
K+/KATP/HA KCNJ1 Mullus auratus 96.0 Radioactive Assay
KAINATE/R GRIK1 Rattus norvegicus 96.0 Radioactive Assay
KAPPA/HU OPRK1 Homo sapiens 74.0 Radioactive Assay
M1/HU CHRM1 Homo sapiens 61.0 Radioactive Assay
M2/HU CHRM2 Homo sapiens 33.0 11.00 48.00 70.00 71.00 108.00 Radioactive Assay
M3/HU CHRM3 Homo sapiens 79.0 Radioactive Assay
MT1/H MTNR1A Homo sapiens 96.0 Radioactive Assay
MU/HU OPRM1 Homo sapiens 91.0 Radioactive Assay
NA+/SITE2/RA SCN1B Rattus norvegicus 60.0 Radioactive Assay
NA+/SITE2AG Cavia porcellus 100.00 antagonist Isometric (gm changes)
NA+/SITE2ATG Cavia porcellus 100.00 antagonist Others
NACH/H CHRNA1 Homo sapiens 102.0 Radioligand Binding
NACH_BS_N/H CHRNA1
 CHRNB1
 		Homo sapiens 100.0 Radioactive Assay
NETRANS/H SLC6A2 Homo sapiens 91.0 Radioactive Assay
NK1/HU TACR1 Homo sapiens 100.0 Radioactive Assay
NMDAAGSI/RA Rattus norvegicus 90.0 agonist Radioactive Assay
NMDAGLSI/RA GRIN1 Rattus norvegicus 109.0 inhibitor Scintillation counting
NMDAPHSI/R GRIN2A Rattus norvegicus 96.0 Radioactive Assay
P2X/RB P2RX1 Oryctolagus cuniculus 98.0 Radioactive Assay
P2Y/RAT P2RY1 Rattus norvegicus 88.0 Radioactive Assay
PHORBOLE/M PRKCA Mus musculus 101.0 inhibitor Radioactive Assay
ROLIPRAM/R PDE4A Rattus norvegicus 92.0 Radioligand Binding
SIGMA1/HU SIGMAR1 Homo sapiens 114.0 Radioactive Assay
SIGMA2/R TMEM97 Rattus norvegicus 90.0 Radioactive Assay
TESTOST/RA AR Rattus norvegicus 95.0 Others
THYROID HORM THRA Rattus norvegicus 93.0 Radioactive Assay
Y1/HU NPY1R Homo sapiens 94.0 Radioactive Assay
Y2/HU NPY2R Homo sapiens 103.0 Radioactive Assay